Abstract:
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
Abstract:
Compounds that bind the glucagon-like peptide 1 receptor (GLP-1) receptor are provided including compounds which are modulators of the GLP-1 receptors and compounds which are capable of inducing a stabilizing effect on the receptor for use in structural analyses of the GLP-1 receptor. Methods of synthesis, methods of therapeutic and/or prophylactic use, and methods of use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor of such compounds are provided.
Abstract:
The present invention provides compounds that are inducers or inhibitors of apoptosis of apoptosis preceded by cell-cycle arrest. In addition, the present invention provides pharmaceutical compositions and methods for treating mammals with leukemia or other forms of cancer or for treating disease conditions caused by apoptosis of cells.
Abstract:
A compound of the general formula (I): (wherein the symbols are as defined in the description), or a non-toxic salt thereof. This compound engages in LPA receptor bonding and antagonism and hence is useful in the prevention and/or treatment of urinary system disease (symptom with prostatic hypertrophy or neurogenic bladder dysfunction disease, symptom to be caused by spinal cord neoplasm, nucleous hernia, spinal canal stenosis or diabetes, occlusion disease of lower urinary tract, inflammatory disease of lower urinary tract, polyuria), carcinoma-associated disease (solid tumor, solid tumor metastasis, angiofibroma, myeloma, multiple myeloma, Kaposi's sarcoma, leucemia and carcinomatous infiltration transition), proliferative disease (disorder with aberrant angiogenesis, artery obstruction and pulmonary fibrosis), inflammation/immune system disease (psoriasis, nephropathy, hepatitis and pneumonitis symptom), disease caused by secretory dysfunction (Sjogren syndrome), brain-related disease (brain infarction, cerebral apoplexy and brain or peripheral neuropathy) or chronic disease (chronic asthma, glomerulonephritis, obesity, prostate hyperplasia, diseases caused by arteriosclerosis process, rheumatism or atopic dermatitis).
Abstract:
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
Abstract:
Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
Abstract:
Thyroid receptor ligands are provided which have the general formula I wherein: R1 is R2 and R3 are the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, provided that at least one of R2 and R3 is other than hydrogen; R4 is R5 and R6 are the same or different and are selected from hydrogen, aryl, heteroaryl, alkyl, cycloalkyl, aralkyl or heteroaralkyl. R7 is aryl, heteroaryl, alkyl, aralkyl, or heteroaralkyl; R8 is aryl, heteroaryl, or cycloalkyl; R9 is R7 or hydrogen; R10 is hydrogen, halogen, cyano or alkyl; R11 and R12 are each independently selected from the group consisting of hydrogen, halogen, alkoxy, hydroxy (—OH) cyano, and alkyl; R13 is carboxylic acid (COOH) or esters thereof, phosphonic and phosphinic acid or esters thereof, sulfonic acid, tetrazole, hydroxamic acid, thiazolidinedione, acylsulfonamide, or other carboxylic acid surrogates known in the art; R14 and R15 may be the same or different and are selected from hydrogen and alkyl, or R14 and R15 may be joined together forming a chain of 2 to 5 methylene groups [—(CH2)m-, m=2, 3, 4 or 5], thus forming 3- to 6-membered cycloalkyl rings; R16 is hydrogen or alkyl of 1 to 4 carbons; R17 and R18 are the same or different and selected from hydrogen, halogen and alkyl; n is 0 or an integer from 1 to 4; X is oxygen (—O—), sulfur (—S—), sulfonyl (—SO2—), sulfenyl (—SO—) selenium (—Se—), carbonyl (—CO—), amino (—NH—) or methylene (—CH2-); wherein the substituents are as described herein. In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.
Abstract translation:提供具有通式I的甲状腺受体配体,其中:R 1是R 2和R 3相同或不同,是氢,卤素,1至4个碳的烷基或3至5个碳原子的环烷基,条件是R2中的至少一个 并且R 3不是氢; R 4是R 5和R 6相同或不同,并且选自氢,芳基,杂芳基,烷基,环烷基,芳烷基或杂芳烷基。 R7是芳基,杂芳基,烷基,芳烷基或杂芳烷基; R8是芳基,杂芳基或环烷基; R9为R7或氢; R 10是氢,卤素,氰基或烷基; R 11和R 12各自独立地选自氢,卤素,烷氧基,羟基(-OH)氰基和烷基; R13是羧酸(COOH)或其酯,膦酸和次膦酸或其酯,磺酸,四唑,异羟肟酸,噻唑烷二酮,酰基磺酰胺或本领域已知的其它羧酸替代物; R 14和R 15可以相同或不同,并且选自氢和烷基,或者R 14和R 15可以连接在一起形成2至5个亚甲基 - [ - (CH 2)m - ,m = 2,3,4或 5],从而形成3-至6-元环烷基环; R16是氢或1至4个碳的烷基; R 17和R 18相同或不同,选自氢,卤素和烷基; n为0或1至4的整数; X是氧(-O-),硫(-S-),磺酰基(-SO 2 - ),亚磺酰基(-SO-),硒(-Se-),羰基(-CO-),氨基(-NH-) 或亚甲基(-CH2-); 其中取代基如本文所述。 此外,提供了一种用于预防,抑制或治疗与代谢功能障碍相关或依赖于T3调节基因的表达的疾病或病症的方法,其中如上所述的化合物以治疗有效量施用。
Abstract:
Provided herein are certain substituted N-phenethylbenzamide of formula V: that may be useful for treating certain cellular proliferation diseases and disorders by modulating the activity of CENP-E.
Abstract:
Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.
Abstract:
Novel biaromatic compounds that modulate peroxisome proliferator-activator receptors, known as PPAR, having the formula (I): are formulated into pharmaceutical compositions useful in human or veterinary medicine, or alternatively, in cosmetic compositions.